AU2004238238C1 - Androgen receptor modulators and methods of use thereof - Google Patents

Androgen receptor modulators and methods of use thereof Download PDF

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Publication number
AU2004238238C1
AU2004238238C1 AU2004238238A AU2004238238A AU2004238238C1 AU 2004238238 C1 AU2004238238 C1 AU 2004238238C1 AU 2004238238 A AU2004238238 A AU 2004238238A AU 2004238238 A AU2004238238 A AU 2004238238A AU 2004238238 C1 AU2004238238 C1 AU 2004238238C1
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AU
Australia
Prior art keywords
methyl
ene
aza
androst
aryl
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Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
AU2004238238A
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English (en)
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AU2004238238B2 (en
AU2004238238A1 (en
Inventor
Robert S. Meissner
James J. Perkins
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Merck Sharp and Dohme LLC
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Merck Sharp and Dohme LLC
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Filing date
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Application filed by Merck Sharp and Dohme LLC filed Critical Merck Sharp and Dohme LLC
Publication of AU2004238238A1 publication Critical patent/AU2004238238A1/en
Publication of AU2004238238B2 publication Critical patent/AU2004238238B2/en
Application granted granted Critical
Publication of AU2004238238C1 publication Critical patent/AU2004238238C1/en
Assigned to MERCK SHARP & DOHME CORP. reassignment MERCK SHARP & DOHME CORP. Request to Amend Deed and Register Assignors: MERCK & CO., INC.
Assigned to MERCK SHARP & DOHME CORP. reassignment MERCK SHARP & DOHME CORP. Request to Amend Deed and Register Assignors: MERCK & CO., INC.
Assigned to MERCK SHARP & DOHME CORP. reassignment MERCK SHARP & DOHME CORP. Request to Amend Deed and Register Assignors: MERCK SHARP & DOHME CORP.
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/26—Androgens
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J73/00—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms
    • C07J73/001—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms by one hetero atom
    • C07J73/005—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms by one hetero atom by nitrogen as hetero atom

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Reproductive Health (AREA)
  • Immunology (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurology (AREA)
  • Dermatology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
AU2004238238A 2003-05-07 2004-05-03 Androgen receptor modulators and methods of use thereof Ceased AU2004238238C1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US46857903P 2003-05-07 2003-05-07
US60/468,579 2003-05-07
PCT/US2004/013787 WO2004100874A2 (fr) 2003-05-07 2004-05-03 Modulateurs du recepteur d'androgenes et leur methode d'utilisation

Publications (3)

Publication Number Publication Date
AU2004238238A1 AU2004238238A1 (en) 2004-11-25
AU2004238238B2 AU2004238238B2 (en) 2009-07-16
AU2004238238C1 true AU2004238238C1 (en) 2010-01-14

Family

ID=33452214

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2004238238A Ceased AU2004238238C1 (en) 2003-05-07 2004-05-03 Androgen receptor modulators and methods of use thereof

Country Status (7)

Country Link
US (2) US7351698B2 (fr)
EP (1) EP1622567B1 (fr)
JP (1) JP4832303B2 (fr)
CN (1) CN1784236A (fr)
AU (1) AU2004238238C1 (fr)
CA (1) CA2524409C (fr)
WO (1) WO2004100874A2 (fr)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102939287B (zh) 2010-06-10 2016-01-27 塞拉根制药公司 雌激素受体调节剂及其用途
US9193714B2 (en) 2011-12-14 2015-11-24 Seragon Pharmaceuticals, Inc. Fluorinated estrogen receptor modulators and uses thereof
NZ710707A (en) 2013-02-08 2016-10-28 Footfalls And Heartbeats Ltd Method for optimizing contact resistance in electrically conductive textiles
CN103405810A (zh) * 2013-08-02 2013-11-27 苏州市马尔泰新材料有限公司 一种含有甲基丙烯酸甲酯树脂的阴道模具
CN103393489A (zh) * 2013-08-02 2013-11-20 苏州市马尔泰新材料有限公司 一种含有雌二醇的阴道模具
CN103431930A (zh) * 2013-08-02 2013-12-11 苏州市马尔泰新材料有限公司 一种含有甲酯树脂的阴道模具
CN103445892A (zh) * 2013-08-02 2013-12-18 苏州市马尔泰新材料有限公司 一种含有甲酯树脂和雌酚的阴道模具
CN103394127A (zh) * 2013-08-02 2013-11-20 苏州市马尔泰新材料有限公司 一种含有中西医药的阴道模具材料
CN103394128A (zh) * 2013-08-02 2013-11-20 苏州市马尔泰新材料有限公司 一种含有川芎的模具材料
WO2015022671A1 (fr) 2013-08-16 2015-02-19 Footfalls And Heartbeats Limited Procédé pour la fabrication de textiles conducteurs d'électricité et capteur textile
CN103694299A (zh) * 2014-01-13 2014-04-02 中国药科大学 甾体类雄激素受体抑制剂、其制备方法及其医药用途
WO2018115879A1 (fr) 2016-12-21 2018-06-28 Mereo Biopharma 3 Limited Utilisation d'anticorps anti-sclérostine dans le traitement de l'ostéogenèse imparfaite
CN108727453A (zh) * 2017-04-20 2018-11-02 华东理工大学 新型pd-1抑制剂及其应用
CA3128468A1 (fr) 2017-10-05 2019-04-11 Fulcrum Therapeutics, Inc. Inhibiteurs de la kinase p38 reduisant l'expression du gene dux4 et des genes aval pour le traitement de la fshd
US10342786B2 (en) 2017-10-05 2019-07-09 Fulcrum Therapeutics, Inc. P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD

Family Cites Families (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4377584A (en) 1978-04-13 1983-03-22 Merck & Co., Inc. 4-Aza-17β-substituted-5α-androstan-3-one-reductase inhibitors
IE76452B1 (en) * 1990-10-29 1997-10-22 Sankyo Co Azasteroid compounds for the treatment of prostatic hypertrophy their preparation and use
ATE183193T1 (de) * 1992-05-20 1999-08-15 Merck & Co Inc 17-amino-substituierte 4-azasteroide als 5-alpha- reductase inhibitoren
WO1993023039A1 (fr) * 1992-05-20 1993-11-25 Merck & Co., Inc. 4-aza-5a-androstan ones substituees utilisees en tant qu'inhibitors de la 5a-reductase
US5620986A (en) 1992-05-20 1997-04-15 Merck & Co., Inc. 17 urea, thiourea, thiocarbamyl and carbamyl4-azasteroid 5-reductase inhibitors useful in the prevention and treatment of hyperandrogenic disorders
US5710275A (en) * 1992-05-20 1998-01-20 Merck & Co., Inc. 7β-substituted-4-aza-5α-androstan-3-ones as 5α-reductase inhibitors
KR950701527A (ko) * 1992-05-21 1995-04-28 라브리 페르낭 테스토스테론 5α 환원효소 활성 저해제(INHIBITORS OF TESTOSTERONE 5α-REDUCTASE ACTIVITY)
HU212459B (en) 1992-10-02 1996-06-28 Richter Gedeon Vegyeszet Process for producing new 17-beta-substituted 4-aza-androstane-derivatives and pharmaceutical compositions containing them
DE69329933T2 (de) * 1992-10-06 2001-07-19 Merck & Co Inc 17-beta-carboxanilid derivate von 4-aza-5-alpha-androstan-3-one als 5-alpha-reduktase-hemmende arzneimittel
US5359071A (en) 1993-03-12 1994-10-25 Merck & Co., Inc. 15-substituted 4-azasteroids
AU681585B2 (en) 1993-06-24 1997-09-04 Richter Gedeon Vegyeszeti Gyar Rt. Novel process for preparing 17beta -substituted 4-azaandrostane derivatives
US5583228A (en) 1993-06-24 1996-12-10 Richter Gedeon Vegyeszeti Gyar Rt. 17-halogeno-4-azaandrostene derivatives and process for the preparation thereof
USRE39056E1 (en) * 1995-09-15 2006-04-04 Merck & Co, Inc. 4-Azasteroids for treatment of hyperandrogenic conditions
WO1997015564A1 (fr) * 1995-10-26 1997-05-01 Merck & Co., Inc. Steroides 4-oxa et 4-thia
BR9708301A (pt) 1996-02-14 1999-08-03 Hoechst Marion Roussel Inc Esteróides de 17-beta-ciclopropil (amino/óxi) 4-aza como inibidores ativos de 5-alfa-redutase e liase de c17-20 de testosterona
WO1998025622A1 (fr) * 1996-12-09 1998-06-18 Merck & Co., Inc. Procedes et compositions permettant la prevention et le traitement de la perte osseuse

Also Published As

Publication number Publication date
CN1784236A (zh) 2006-06-07
JP2006528686A (ja) 2006-12-21
EP1622567A4 (fr) 2009-04-29
US20080119503A1 (en) 2008-05-22
US7351698B2 (en) 2008-04-01
JP4832303B2 (ja) 2011-12-07
EP1622567A2 (fr) 2006-02-08
AU2004238238B2 (en) 2009-07-16
CA2524409C (fr) 2011-12-20
CA2524409A1 (fr) 2004-11-25
WO2004100874A2 (fr) 2004-11-25
AU2004238238A1 (en) 2004-11-25
US20060241107A1 (en) 2006-10-26
WO2004100874A3 (fr) 2006-01-26
EP1622567B1 (fr) 2013-07-24

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Legal Events

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DA2 Applications for amendment section 104

Free format text: THE NATURE OF THE AMENDMENT IS AS SHOWN IN THE STATEMENT(S) FILED 25 AUG 2009.

DA3 Amendments made section 104

Free format text: THE NATURE OF THE AMENDMENT IS AS SHOWN IN THE STATEMENT(S) FILED 25 AUG 2009

DA3 Amendments made section 104

Free format text: THE NATURE OF THE AMENDMENT IS: AMEND THE PATENTEE FROM MERCK & CO., INC. TO MERCK SHARP & DOHME CORP.

FGA Letters patent sealed or granted (standard patent)
MK14 Patent ceased section 143(a) (annual fees not paid) or expired